专利号:WO-2024185734-A1 优先权日:2023-03-03 标 题:Polyphosphorylated nucleoside, phosphate-activated nucleotide used for synthesis of polyphosphorylated nucleoside and method for synthesis of same, and method for synthesis of polyphosphorylated nucleoside using phosphate-activated nucleotide 发明人:KATAOKA MASANORI; FUKUI CHIHARU; TSUJI YOHEI; FUJIMURA Kazuma 权利人:NATIAS INC 摘要:The present invention provides: a polyphosphorylated nucleoside which has a structure represented by formula (I) and can be efficiently produced by a short process and a simple operation with use of a less expensive material; a phosphate-activated nucleotide which is used for the synthesis of the polyphosphorylated nucleoside and a method for the synthesis of this phosphate-activated nucleotide; and a method for the synthesis of a polyphosphorylated nucleoside using a phosphate-activated nucleotide. In the formula, B represents a protected or unprotected, natural or artificial nucleoside base; R 1 , R 2 , R 4 and R 5 each represent H or an alkyl group or the like, and R 1 , R 2 , R 4 and R 5 may be the same as or different from each other; X and Y each represents H, OH, OCH 3 or the like; h represents an integer of 1 to 3; p, n, m and q each represent 0 or an integer, and p, n, m and q are in no particular order; and (p + n + m + q) is an integer of 0 to 5,000.
专利号:US-12240835-B2 优先权日:2018-09-18 标题:Substituted benzamides as intermediates in the synthesis of inhibitors of tyrosine kinase enzymatic activity 发明人:ROMERO F ANTHONY; KIRSCHBERG THORSTEN A; HALCOMB RANDALL; XU YINGZI 权利人:TERNS PHARMACEUTICALS INC 摘要:Provided herein are compounds, preferably compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, compositions thereof, and methods of their preparation, and methods of inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, and methods for treating diseases wherein modulation of BCR-ABL1 activity prevents, inhibits, or ameliorates the pathology and/or symptomology of the disease. Intermediates such as compounds of Formula (S23), which are useful in the synthesis of compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, are also provided.
专利号:US-6384228-B2 优先权日:1998-05-26 标题 :Method for synthesis of halopyridyl-azacyclopentane derivative and intermediate thereof 发明人:NODE MANABU; NAKAMURA DAISAKU; FUJIWARA TOSHIO; ICHIHASHI SHOGO 权利人:NIHON MEDIPHYSICS CO LTD 摘要:The present invention relates to a method for synthesis of an optically active halopyridyl-azacyclo-pentane derivative and the intermediate thereof which comprises preparing an optically active allene-1,3-dicarboxylic acid ester derivative from an optically active acetonedicarboxylic acid ester derivative and then proceeding through a 7-azabicyclo[2.2.1]heptane derivative to obtain the objective product.
专利号:US-2010159540-A1 优先权日:2007-03-26 标题:Synthesis of resolvins and intermediates, compounds prepared thereby, and uses thereof 发明人:RODRIGUEZ ANA; SPUR BERND 权利人:RODRIGUEZ ANA; SPUR BERND 摘要:Methods are disclosed for the preparation of a new class of lipid mediators known as resolvins, with Resolvin D6 (4,17-dihydroxy-5E,7Z,10Z,13Z,15E,19Z-docosahexaenoic acid) being exemplary. Also disclosed are methods for the efficient synthesis of key intermediates in the preparation of such resolvins, such as isotopically labeled ω-3 fatty acid metabolites, and derivatives and analogs thereof. The invention likewise extends to the intermediates so prepared, and to the resolvins prepared with their use.
专利号:US-9938282-B2 优先权日:2014-02-05 标 题:Expedient synthesis of sitagliptin 发明人:JANAGANI SATYANARAYANA; THADURI VENKATESHWAR KUMAR; VAMARAJU RAVISANKAR 权利人:STEREOKEM INC 摘要:Novel intermediates are disclosed as intermediates for preparation of a Sitagliptin. A novel synthetic method to prepare Sitagliptin using the said intermediates is also disclosed.
专利号:US-8063062-B2 优先权日:2006-12-20 标 题 :Compounds with a combination of cannabinoid-CB1 antagonism and acetylcholinesterase inhibition 发明人:LANGE JOSEPHUS H M; KRUSE CORNELIS G; SHADID BELAL 权利人:LANGE JOSEPHUS H M; KRUSE CORNELIS G; SHADID BELAL; SOLVAY PHARM BV 摘要:Embodiments of this invention relate to compounds having a combination of cannabinoid-CB 1 antagonism and cholinesterase inhibition, to pharmaceutical compositions comprising these compounds, to methods for preparing these compounds, methods for preparing novel intermediates useful for the synthesis of these compounds, and methods for preparing compositions comprising these compounds. The invention also relates to methods of treating Alzheimer's disease, cognitive disorders, memory disorders, dementia, attention deficit disorder, traumatic brain injury, drug dependence, addiction or substance abuse by administering a pharmaceutical composition comprising these compounds to a patient in need thereof. A compound with a combination of cannabinoid-CB 1 antagonism and cholinesterase inhibition is a compound of formula (1) n nwherein the symbols have the meanings given in the specification.
[参考文献]: Alois Fürstner, Et Al. Structure Assignment, Total Synthesis, And Antiviral Evaluation Of Cycloviracin B1. J Am Chem Soc. 2003 Oct 29;125(43):13132-42. [参考文献]: Shunya Takahashi, Et Al. Synthetic Studies On Macroviracin A: A Rapid Construction Of C(42) Macrocyclic Dilactone Corresponding To The Core. J Org Chem. 2004 Jun 25;69(13):4509-15.
合成参考文献
摘要:Gandon, V.; Malacria, M., Science of Synthesis, (2008) 44, 222. 摘要:Pajkert, R.; Röschenthaler, G.-V., Science of Synthesis Knowledge Updates, (2022) 1, 407.